EP 1723141 A4 20071010 - INDUSTRIAL PROCESS FOR PREPARATION OF CLOPIDOGREL HYDROGEN SULPHATE
Title (en)
INDUSTRIAL PROCESS FOR PREPARATION OF CLOPIDOGREL HYDROGEN SULPHATE
Title (de)
GROSSTECHNISCHES VERFAHREN ZUR HERSTELLUNG VON CLOPIDOGRELHYDROGENSULFAT
Title (fr)
PROCEDE INDUSTRIEL DE FABRICATION DE SULFATE D'HYDROGENE DE CLOPIDROGREL
Publication
Application
Priority
- IN 2005000071 W 20050304
- IN 281MU2004 A 20040305
- IN 626MU2004 A 20040604
- IN 861MU2004 A 20040810
Abstract (en)
[origin: WO2005104663A2] An improved process for the manufacture of Clopidogrel starting from 2-(2-thienyl) ethylamine, which eliminates the isolation of an unstable intermediate like 2-(2-thienyl) ethyl formimine by subjecting it to a one pot cyclization to get 4, 5, 6, 7-tetrahydrothieno (3,2-c) pyridine of Formula II and further reacting with halo-compound of Formula III (where X is C1 or Br) at 20 to 90 <°>C temperature characterized in a solvent like water and/or dichloroethane in presence of organic or inorganic bases is disclosed herein. This invention further discloses a process for resolution of racemic Clopidogrel into its optical antipodes and converting the dextroclopidogrel base into its known polymorphs namely 'Form I' or 'Form II' in solvents selected from methyl propyl ketone, methyl isopropyl ketone, diethyl ketone or their mixture thereof, mixture of ethyl acetate and methyl propyl ketone, mixture of ethyl acetate and methyl isopropyl ketone, or mixture of ethyl acetate and diethyl ketone or ethyl acetate.
IPC 8 full level
C07D 409/04 (2006.01); C07D 495/04 (2006.01)
CPC (source: EP US)
C07D 495/04 (2013.01 - EP US)
Citation (search report)
- [Y] US 5068360 A 19911126 - DEHOFF BRADLEY S [US]
- [Y] EP 0439404 A2 19910731 - SANOFI SA [FR]
- [X] US 6429210 B1 20020806 - BOUSQUET ANDRE [FR], et al
- See references of WO 2005104663A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU MC NL PL PT RO SE SI SK TR
DOCDB simple family (publication)
WO 2005104663 A2 20051110; WO 2005104663 A3 20060928; EP 1723141 A2 20061122; EP 1723141 A4 20071010; EP 1772455 A2 20070411; EP 1772455 A3 20070627; US 2008097101 A1 20080424; US 2010160635 A1 20100624; US 7629465 B2 20091208
DOCDB simple family (application)
IN 2005000071 W 20050304; EP 05767878 A 20050304; EP 06120928 A 20050304; US 59165705 A 20050304; US 60771409 A 20091028